Patents by Inventor Shane W. Krska

Shane W. Krska has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for the Prepartion of an Orexin Receptor Antagonist
    Publication number: 20210309650
    Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
    Type: Application
    Filed: July 16, 2015
    Publication date: October 7, 2021
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
  • Process for making M1 receptor positive allosteric modulators
    Patent number: 10308633
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: June 4, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • PROCESS FOR MAKING M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20180265493
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 20, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited.
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • COMPOUND DIVERSIFICATION USING LATE STAGE FUNCTIONALIZATION
    Publication number: 20150274755
    Abstract: The present invention relates to methods for generating limited chemical diversity for biologically relevant lead molecules by late state functionalization, separation, and post-functionalization modification. The methods optionally include one or more screening steps. Traditional drug development has relied on the synthesis of individual compounds or the generation of large chemical libraries, but these methods have generally been fairly inefficient in obtaining drug products.
    Type: Application
    Filed: September 20, 2013
    Publication date: October 1, 2015
    Inventors: Shane W. Krska, Petr Vachal, Christopher J. Welch, Graham F. Smith
  • Process for the preparation of an orexin receptor antagonist
    Patent number: 9108959
    Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: August 18, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
  • PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST
    Publication number: 20130331379
    Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.
    Type: Application
    Filed: February 27, 2012
    Publication date: December 12, 2013
    Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
  • Process for the preparation of enantiomerically enriched beta amino acid derivatives
    Patent number: 7495123
    Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: February 24, 2009
    Assignees: Solvias AG, Merck & Co., Inc.
    Inventors: Yi Xiao, Yongkui Sun, Thorsten Rosner, Nelo R. Rivera, Shane W. Krska, Andrew M. Clausen, Joseph D. Armstrong, III, Felix Spindler, Christophe Malan
  • Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
    Patent number: 7468459
    Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.
    Type: Grant
    Filed: March 15, 2004
    Date of Patent: December 23, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Yi Xiao, Joseph D. Armstrong, III, Shane W. Krska, Eugenia Njolito, Nelo R. Rivera, Yongkui Sun, Thorsten Rosner
  • Process for a carbon-carbon coupling reaction of aryl halides with olefins by heterogeneous catalysts
    Publication number: 20020128478
    Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.
    Type: Application
    Filed: March 4, 2002
    Publication date: September 12, 2002
    Inventors: Shane W. Krska, Thorsten S. Rosner, Yongkui Sun